Assay Detail
Binding
CHEMBL5732654
Review assay metadata, readout intent, target linkage, and publication context from the same page.
AlphaLisa Binding Assay: His/Flag epitope tagged BRD4 BD142-168 was cloned, expressed, and purified to. BRD4 binding and inhibition was assessed by monitoring the engagement of biotinylated H4-tetraacetyl peptide (New England Peptide, NEP2069-1/13) with the target using the AlphaLisa technology (Perkin-Elmer). Specifically, in a 384 well ProxiPlate BRD4(BD1) (30 nM final) was combined with peptide (200 nM final) in 40 mM HEPES (pH 7.0), 40 mM NaCl, 1 mM DTT, 0.01% (w/v) BSA, and 0.008% (w/v) Brij-35 either in the presence of DMSO (final 1.2% DMSO) or compound dilution series in DMSO. After 20 minutes incubation at room temperature Alpha streptavidin donor beads and AlphaLisa anti-Flag acceptor beads were added to a final concentration of 10 ug/mL each. After three hours equilibration plates were read on an Envision instrument and IC50s calculated using a four parameter non-linear curve fit.
855
Total Activities
283
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Therapeutic compounds and uses thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 285 | 5.32 | 6.12 |
| kon | 285 | - | - |
| k_off | 285 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5788497 | — | — | 3 | 6.12 |
| CHEMBL3962542 | — | — | 3 | 6.08 |
| CHEMBL5932721 | — | — | 3 | 6.05 |
| CHEMBL5915732 | — | — | 3 | 6.05 |
| CHEMBL5978449 | — | — | 3 | 5.99 |
| CHEMBL3893541 | — | — | 3 | 5.94 |
| CHEMBL6057802 | — | — | 3 | 5.92 |
| CHEMBL5786314 | — | — | 3 | 5.90 |
| CHEMBL5739795 | — | — | 3 | 5.87 |
| CHEMBL5850494 | — | — | 3 | 5.82 |
| CHEMBL5763429 | — | — | 3 | 5.81 |
| CHEMBL6030015 | — | — | 3 | 5.80 |
| CHEMBL6034588 | — | — | 3 | 5.78 |
| CHEMBL6051302 | — | — | 3 | 5.77 |
| CHEMBL5785255 | — | — | 3 | 5.77 |
| CHEMBL5797284 | — | — | 3 | 5.75 |
| CHEMBL5878573 | — | — | 3 | 5.71 |
| CHEMBL5993926 | — | — | 3 | 5.71 |
| CHEMBL5755667 | — | — | 3 | 5.71 |
| CHEMBL5988786 | — | — | 3 | 5.70 |
| CHEMBL3973515 | — | — | 3 | 5.70 |
| CHEMBL5799756 | — | — | 3 | 5.70 |
| CHEMBL5844745 | — | — | 3 | 5.70 |
| CHEMBL3981511 | — | — | 3 | 5.68 |
| CHEMBL5861031 | — | — | 3 | 5.68 |
| CHEMBL5778340 | — | — | 3 | 5.67 |
| CHEMBL5849184 | — | — | 3 | 5.67 |
| CHEMBL6013447 | — | — | 3 | 5.67 |
| CHEMBL5997292 | — | — | 3 | 5.66 |
| CHEMBL5994636 | — | — | 3 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5788497 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL3962542 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL5915732 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL5932721 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL5978449 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL3893541 | — | IC50 | = | 1160.0 | nM | 5.94 |
| CHEMBL6057802 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5786314 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL5739795 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL5850494 | — | IC50 | = | 1510.0 | nM | 5.82 |
| CHEMBL5763429 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL6030015 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL6034588 | — | IC50 | = | 1680.0 | nM | 5.78 |
| CHEMBL6051302 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL5785255 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL5797284 | — | IC50 | = | 1790.0 | nM | 5.75 |
| CHEMBL5878573 | — | IC50 | = | 1970.0 | nM | 5.71 |
| CHEMBL5993926 | — | IC50 | = | 1930.0 | nM | 5.71 |
| CHEMBL5755667 | — | IC50 | = | 1930.0 | nM | 5.71 |
| CHEMBL3973515 | — | IC50 | = | 2020.0 | nM | 5.70 |
| CHEMBL5988786 | — | IC50 | = | 1980.0 | nM | 5.70 |
| CHEMBL5799756 | — | IC50 | = | 1990.0 | nM | 5.70 |
| CHEMBL5844745 | — | IC50 | = | 1980.0 | nM | 5.70 |
| CHEMBL3981511 | — | IC50 | = | 2110.0 | nM | 5.68 |
| CHEMBL5861031 | — | IC50 | = | 2080.0 | nM | 5.68 |
| CHEMBL5849184 | — | IC50 | = | 2130.0 | nM | 5.67 |
| CHEMBL6013447 | — | IC50 | = | 2140.0 | nM | 5.67 |
| CHEMBL5778340 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL5997292 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5922716 | — | IC50 | = | 2180.0 | nM | 5.66 |
| CHEMBL5994636 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5759913 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL5976442 | — | IC50 | = | 2360.0 | nM | 5.63 |
| CHEMBL5819653 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL5780329 | — | IC50 | = | 2330.0 | nM | 5.63 |
| CHEMBL5885467 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL5857985 | — | IC50 | = | 2410.0 | nM | 5.62 |
| CHEMBL5856964 | — | IC50 | = | 2450.0 | nM | 5.61 |
| CHEMBL5898021 | — | IC50 | = | 2460.0 | nM | 5.61 |
| CHEMBL5822280 | — | IC50 | = | 2480.0 | nM | 5.61 |
| CHEMBL3911524 | — | IC50 | = | 2470.0 | nM | 5.61 |
| CHEMBL5970105 | — | IC50 | = | 2520.0 | nM | 5.60 |
| CHEMBL5909280 | — | IC50 | = | 2490.0 | nM | 5.60 |
| CHEMBL6024359 | — | IC50 | = | 2490.0 | nM | 5.60 |
| CHEMBL6036457 | — | IC50 | = | 2520.0 | nM | 5.60 |
| CHEMBL3924330 | — | IC50 | = | 2540.0 | nM | 5.59 |
| CHEMBL3892467 | — | IC50 | = | 2630.0 | nM | 5.58 |
| CHEMBL5991421 | — | IC50 | = | 2650.0 | nM | 5.58 |
| CHEMBL5963804 | — | IC50 | = | 2630.0 | nM | 5.58 |
| CHEMBL5828833 | — | IC50 | = | 2610.0 | nM | 5.58 |